Bupivacaine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Parenteral
Acute pain
Adult: Lumbar block in labour pain: 0.25% soln: 15-30 mg (6-12 mL); 0.375% soln: 22.5-45 mg (6-12 mL); 0.5% soln: 30-60 mg (6-12 mL). Alternatively, 0.1% soln: 10-15 mg (10-15 mL) per hr; 0.125% soln: 10-15 mg (8-12 mL) per hr via infusion. Caudal block in labour pain: 0.25% soln: 25-50 mg (10-20 mL); 0.375% soln: 37.5-75 mg (10-20 mL); 0.5% soln: 50-100 mg (10-20 mL).
Child: 1-12 yr Caudal/Lumbar/Thoracic epidural block: 0.25% soln: 1.5-2 mg/kg. Field block/Peripheral nerve block: 0.25 or 0.5% soln: 0.5-2 mg/kg.

Parenteral
Postoperative pain
Adult: 0.1% soln: 4-15 mg (4-15 mL) per hr; 0.125% soln: 5-15 mg (4-12 mL) per hr via epidural infusion. 1.3% liposomal susp: Bunionectomy: 106 mg (8 mL) as single dose (7 mL into surrounding tissues and 1 mL into SC tissue); haemorrhoidectomy: 266 mg (20 mL) as single dose, diluted to 30 mL preservative-free 0.9% NaCl for inj and infiltrated around the anal sphincter in 6 equally-divided portions.

Parenteral
Surgical anaesthesia
Adult: Local infiltration: 0.25% soln: Up to 150 mg (60 mL). Peripheral nerve block: 0.25% soln: 12.5 mg (5 mL); 0.5% soln: 25 mg (5 mL); doses of up to 150 mg may also be given. Retrobulbar block in ophth surgery: 0.75% soln: 15-30 mg (2-4 mL). Sympathetic nerve block: 0.25% soln: 50-125 mg (20-50 mL). Lumbar epidural block: 0.25% soln: 25-50 mg (10-20 mL); 0.5% soln: 50-100 mg (10-20 mL); 0.75% soln in non-obstetric surgery: 75-150 mg (10-20 mL) as single dose. Caudal block: 0.25% soln: 37.5-75 mg (15-30 mL); 0.75% soln: 75-150 mg (15-30 mL). Spinal block: 0.5% soln: 10-20 mg (2-4 mL).
Chống chỉ định
Patient w/ active CNS disease (e.g. meningitis, intracranial haemorrhage), TB of the spine, pyogenic infection on inj site, pre-anaesth elevated intracranial pressure. Not intended for IV regional anaesth (Bier's block) and paracervical block in obstetrics; obstetric epidural block (0.75% soln).
Thận trọng
Patient w/ partial or complete heart block, impaired CV function and hypovolaemia; marked obesity, senility, cerebral atheroma, myocardial degeneration, toxaemia (epidural and spinal anaesth). May cause chondrolysis when given via intra-articular continuous infusion. Severe hepatic impairment. Pregnancy and lactation.
Phản ứng phụ
Bradycardia, hypotension, HTN, nausea, vomiting, diplopia, neuropathy, peripheral nerve injury, arachnoiditis, paresis and paraplegia, signs of CNS toxicity (e.g. convulsions, paraesthesia, tremor), dizziness, allergic reactions.
Potentially Fatal: Cardiac arrhythmia, cardiac and resp arrest.
Epidural/Intraspinal/IT/Parenteral/Perineural/SC: C
Thông tin tư vấn bệnh nhân
May temporarily impair locomotion and alertness.
Monitoring Parameters
Monitor CV and resp vital signs, state of consciousness, signs of CNS toxicity.
Quá liều
Symptoms: Convulsions, circulatory arrest, cardiac arrest, resp paralysis, hypotension, bradycardia. Management: Establish and maintain a patent airway, oxygen may be needed. If necessary, may give anticonvulsant drugs.
Tương tác
Additive systemic toxic effect w/ other local anaesth or agents structurally related to amide-type local anaesth (e.g. lidocaine and mexiletine). Increased risk of myocardial depression w/ antiarrhythmics. Enhanced adverse effects w/ hyaluronidase. Decreased clearance resulting to increased plasma concentrations w/ cimetidine and ranitidine. Increased risk of adverse effects w/ β-blockers and Ca channel blockers.
Tác dụng
Description: Bupivacaine blocks both the initiation and conduction of nerve impulses reducing the permeability of neuronal membranes to Na ions resulting in inhibition of depolarization w/ resultant blockade of conduction.
Onset: 1-17 min (route and dose dependent).
Duration: 2-9 hr (route and dose dependent).
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 30-45 min.
Distribution: Crosses the placenta, diffuses into CSF and enters breast milk (small amounts). Plasma protein-binding: Approx 95%.
Metabolism: Hepatic via conjugation w/ glucuronic acid; converted to pipecoloxylidine (major metabolite).
Excretion: Via urine mainly as metabolites; 5-6% as unchanged drug. Half-life: 1.5-5.5 hr
Bảo quản
Soln for inj: Store between 20-25°C. Protect from light; Liposomal susp: Store between 2-8°C.
Phân loại MIMS
References
Anon. Bupivacaine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 25/07/2014.

Buckingham R (ed). Bupivacaine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/07/2014.

Exparel Injection, Suspension, Liposomal (Pacira Pharmaceuticals Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 25/07/2014.

Wickersham RM. Bupivacaine HCl Injection. Facts and Comparisons [online]. St. Louis, MO. Wolters Kluwer Clinical Drug Information, Inc. https://www.wolterskluwercdi.com/facts-comparisons-online/. Accessed 25/07/2014.

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